scholarly journals STUDY OF ANTISECRETORY ACTIVITY OF DINITRATE 2-PHENYL-9-DIETHYLAMINOETHYLimidazo[1,2-A] BENZIMIDAZOLE BY METHOD OF CONTINUOUS PERFUSION OF RATS’ STOMACHS

2019 ◽  
Vol 7 (4) ◽  
pp. 231-240
Author(s):  
M. V. Chernikov ◽  
M. A. Oganova ◽  
A. S. Gerasimenko ◽  
E. A. Artemyev
Keyword(s):  
Hydrochloric Acid ◽  
Dosage Form ◽  
Sodium Hydroxide Solution ◽  
Gastrointestinal Diseases ◽  
New Drugs ◽  
Reference Object ◽  
Reference Drug ◽  
Antisecretory Activity ◽  
Antisecretory Effect ◽  
Continuous Perfusion

Nowadays, effective pharmacotherapy of acid-dependent gastrointestinal diseases remains an urgent problem of modern gastroenterology. In this regard, the search for new drugs with a pronounced antisecretory activity still continues; their aim is to keep the control over the acid production safe and effective.The aim of this study was an experimental study of the antisecretory activity of the substance and the finished dosage form (FDF) of dinitrate 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole.Materials and Methods. The study of antisecretory activity was performed by method of a continuous perfusion of rats’ stomachs. The studied substance was administered at the doses of 3, 10 and 30 mg/kg, and the FDF – at the doses of 13 and 26 mg/kg. The substance of Ranitidine (Sigma Аldrich, USA) was used as a reference object in the study of the antisecretory activity of the substance under study, and Ranitidine (Hemofarm A.D., Serbia) was used as a reference drug in the study of the FDF. In order to determine the stimulated secretion immediately before collecting the samples of the perfusate, histamine was administered subcutaneously at the dose of 5 mg/kg. The content of hydrochloric acid in the perfusate was determined by titration of a 0.01 M sodium hydroxide solution. The acidity value was determined in terms of the debit-hour of hydrochloric acid.Results and discussion. The obtained experimental data showed that the studied substance at the dose of 30 mg/kg decreased the basal hydrochloric acid secretion by 54%, which significantly exceeded the antisecretory effect of Ranitidine by 1.8 times. The FDF at the dose of 26 mg/kg, statistically reliable relative to the control and the group treated with Ranitidine, decreased the basal secretion of gastric juice by 33%. The substance at the dose of 30 mg/kg reliably suppressed the stimulated secretion of hydrochloric acid by 80%, while Ranitidine did it by 56%. The FDF at the dose of 26 mg/kg decreased the histamine-stimulated secretion by 66%, and Ranitidine did it by 52%, which was statistically reliable.Сonclusions. The studied substance and its dosage form are more effective in suppressing basal activities and exceed the anisecretory activity of H2 -histamine antagonists of Ranitidine under the conditions of the secretion stimulated by histamine.

scholarly journals Antimicrobial, Antioxidant, Anti-Acetylcholinesterase, Antidiabetic, and Pharmacokinetic Properties of Carum carvi L. and Coriandrum sativum L. Essential Oils Alone and in Combination

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3625
Author(s):  
Hafedh Hajlaoui ◽  
Soumaya Arraouadi ◽  
Emira Noumi ◽  
Kaïss Aouadi ◽  
Mohd Adnan ◽  
...  
Keyword(s):  
Essential Oils ◽  
Coriandrum Sativum ◽  
New Drugs ◽  
Antidiabetic Activity ◽  
Pharmacokinetic Analysis ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Reference Drug ◽  
Antioxidant Power ◽  
Carum Carvi

Herbs and spices have been used since antiquity for their nutritional and health properties, as well as in traditional remedies for the prevention and treatment of many diseases. Therefore, this study aims to perform a chemical analysis of both essential oils (EOs) from the seeds of Carum carvi (C. carvi) and Coriandrum sativum (C. sativum) and evaluate their antioxidant, antimicrobial, anti-acetylcholinesterase, and antidiabetic activities alone and in combination. Results showed that the EOs mainly constitute monoterpenes with γ-terpinene (31.03%), β-pinene (18.77%), p-cymene (17.16%), and carvone (12.20%) being the major components present in C. carvi EO and linalool (76.41%), γ-terpinene (5.35%), and α-pinene (4.44%) in C. sativum EO. In comparison to standards, statistical analysis revealed that C. carvi EO showed high and significantly different (p < 0.05) antioxidant activity than C. sativum EO, but lower than the mixture. Moreover, the mixture exhibited two-times greater ferric ion reducing antioxidant power (FRAP) (IC50 = 11.33 ± 1.53 mg/mL) and equipotent chelating power (IC50 = 31.33 ± 0.47 mg/mL) than the corresponding references, and also potent activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC50 = 19.00 ± 1.00 mg/mL), β-carotene (IC50 = 11.16 ± 0.84 mg/mL), and superoxide anion (IC50 = 10.33 ± 0.58 mg/mL) assays. Antimicrobial data revealed that single and mixture EOs were active against a panel of pathogenic microorganisms, and the mixture had the ability to kill more bacterial strains than each EO alone. Additionally, the anti-acetylcholinesterase and α-glucosidase inhibitory effect have been studied for the first time, highlighting the high inhibition effect of AChE by C. carvi (IC50 = 0.82 ± 0.05 mg/mL), and especially by C. sativum (IC50 = 0.68 ± 0.03 mg/mL), as well as the mixture (IC50 = 0.63 ± 0.02 mg/mL) compared to the reference drug, which are insignificantly different (p > 0.05). A high and equipotent antidiabetic activity was observed for the mixture (IC50 = 0.75 ± 0.15 mg/mL) when compared to the standard drug, acarbose, which is about nine times higher than each EO alone. Furthermore, pharmacokinetic analysis provides some useful insights into designing new drugs with favorable drug likeness and safety profiles based on a C. carvi and C. sativum EO mixture. In summary, the results of this study revealed that the combination of these EOs may be recommended for further food, therapeutic, and pharmaceutical applications, and can be utilized as medicine to inhibit several diseases.

Cytoprotective and antisecretory properties of methanolic extract of Distemonanthus benthamianus (Caesalpiniaceae) stem bark on acute gastric ulcer in rats

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Vanessa Mba Matah Marthe ◽  
Gilbert Ateufack ◽  
Marius Mbiantcha ◽  
William Yousseu Nana ◽  
Albert Donatien Atsamo ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
Gastric Lesion ◽  
Stem Bark ◽  
Male Rats ◽  
Gastric Ulcers ◽  
Gastric Lesions ◽  
Mucus Production ◽  
Antisecretory Activity ◽  
Antisecretory Effect ◽  
Pylorus Ligation

AbstractObjectivesIn African traditional medicine, Distemonanthus benthamianus (Caesalpiniaceae) is used to treat many diseases including gastric ulcers. We evaluated in this study, the cytoprotective and antisecretory properties of the methanolic extract of the stem bark of this plant using different technics of gastric lesion induction.MethodsCytoprotective and antisecretory activity of the methanolic extract of D. benthamianus stem bark was evolved through six methods of gastric lesion induction in experimental Wistar male rats (150–200 g): (1) gastric lesions induced by HCl/ethanol, (2) gastric lesions induced by Indomethacin- HCl/ethanol, (3) gastric lesion induced by Indomethacin, (4) gastric lesions induced by Pylorus ligation, (5) gastric lesions induced by histamine-Pylorus ligation, (6) gastric lesions induced by carbachol-Pylorus ligation. Mucus and gastric mucosal ulceration were evaluated. pH, gastric volume, and acidity were quantified in all pylorus ligation induction technics. Nitric oxide (NO) level was determined in indomethacin induced gastric ulcers.ResultsAt different doses (125, 250 and 500 mg/kg), extract reduced significantly the ulcer index. In all models used, that is 100.00% with HCl/ethanol; 100.00% with HCl/ethanol/indomethacin; 95.70% with Indomethacin; 74.79% with pylorus ligation, 95.94% histamine-Pylorus ligation, 99.54% carbachol-Pylorus ligation at the highest dose of 500 mg/kg. The lesion formation reduces in all the methods used followed by a significant increase of mucus production. The pylorus ligation technic revealed that the extract has an antisecretory activity.ConclusionsThe methanolic extract of D. benthamianus stem bark has both cytoprotective and antisecretory effects. This extract exerts its antisecretory effect trough cholinergic and histaminergic pathways.

scholarly journals Evaluation of Novel Chalcone-Thiosemicarbazones Derivatives as Potential Anti-Leishmania amazonensis Agents and Its HSA Binding Studies

Biomolecules ◽  
2019 ◽  
Vol 9 (11) ◽  
pp. 643
Author(s):  
Mendes ◽  
Goulart ◽  
Chaves ◽  
Faiões ◽  
Canto-Carvalho ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Selectivity Index ◽  
New Drugs ◽  
Spectroscopic Techniques ◽  
Binding Studies ◽  
Reference Drug ◽  
Intracellular Amastigotes ◽  
Axenic Amastigotes ◽  
Ic50 Values ◽  
Pharmacokinetic Evaluation

A series of seven chalcone-thiosemicarbazones (5a–5g) were synthesized and evaluated as potential new drugs (anti-leishmanial effect). Although four of the chalcone-thiosemicarbazones are already known, none of them or any compound in this class has been previously investigated for their effects on parasites of the Leishmania genus. The compounds were prepared in satisfactory yields (40–75%) and these compounds were evaluated against promastigotes, axenic amastigotes and intracellular amastigotes of L. amazonensis after 48 h of culture. The half maximal inhibitory concentration (IC50) values of the intracellular amastigotes were determined to be in the range of 3.40 to 5.95 µM for all compounds assayed. The selectivity index showed value of 15.05 for 5a, whereas pentamidine (reference drug) was more toxic in our model (SI = 2.32). Furthermore, to understand the preliminary relationship between the anti-leishmanial activity of the chalcone-thiosemicarbazones, their electronic (σ), steric (MR) and lipophilicity (π) properties were correlated, and the results indicated that moieties with electronic withdrawing effects increase the anti-leishmanial activity. The preliminary pharmacokinetic evaluation of one of the most active compound (5e) was studied via interaction to human serum albumin (HSA) using multiple spectroscopic techniques combined with molecular docking. The results of antiparasitic effects against L. amazonensis revealed the chalcone-thiosemicarbazone class to be novel prototypes for drug development against leishmaniasis.

scholarly journals Mouse model of DNCB-induced atopic dermatitis

2017 ◽  
Vol 12 (2) ◽  
pp. 30
Author(s):  
Alshammari Fanar Hamad ◽  
Jong-Hun Han ◽  
Irfan Ahmad Rather
Keyword(s):  
Animal Model ◽  
Atopic Dermatitis ◽  
Video Clip ◽  
Skin Inflammation ◽  
New Drugs ◽  
Dorsal Skin ◽  
Reference Drug ◽  
Allergic Skin ◽  
Full Screen ◽  
Selection Of

<p>Atopic dermatitis is a skin disease characterized by allergic skin inflammation, redness and itching. The animal model is necessary to find out new drugs. The DNCB-induced animal model of atopic dermatitis includes the following steps: 1) Selection of animals; 2) Shaving of dorsal skin; 3) Applying DNCB once in 24 hours for three days; 4) Monitoring the development of atopy on day 4 post DNCB application. Further, the efficacy of reference drug can be determined by applying on the atopy skin, depends on the nature and aim of the work.</p><p><strong>Video Clip of Methodology</strong>: 8 min   <a href="https://www.youtube.com/v/XbFt1bOnulc">Full Screen</a>   <a href="https://www.youtube.com/watch?v=XbFt1bOnulc">If Failed</a></p>

scholarly journals Study of wound-healing activity of sodium 2-(adamantane-1-yl)-2-hydrazino-5-phenyl-4-oxobutanoate

2021 ◽  
Vol 38 (6) ◽  
pp. 69-73
Author(s):  
Alexander S. Kuznetsov ◽  
Natalya A. Pulina ◽  
Svetlana V. Chashchina
Keyword(s):  
Wound Healing ◽  
Sodium Alginate ◽  
Dosage Form ◽  
Practical Application ◽  
Chemical Methods ◽  
Reference Drug ◽  
Pharmaceutical Substance ◽  
White Rats ◽  
Complex Wound ◽  
Wound Healing Activity

Objective. To study a wound-healing activity of the earlier synthesized compound-leader sodium 2- (adamantan-1-yl)-2-hydrazino-5-phenyl-4-oxobutenoate (1), as well as to establish the possibility of its practical application in the ointment dosage form. Materials and methods. The substance-leader 1 was synthesized by the chemical methods described earlier. The experimental 5 % ointment composition based on an aqueous solution of sodium alginate was developed in compliance with the rules for preparing homogeneous ointments. Its effect on the healing of linear aseptic skin wounds in white rats was studied by the method of wound-tensiometry. Results. The experimental 5 % ointment composition with compound 1 was found to significantly increase the scar tensile strength compared to control without treatment. The developed model ointment showed wound-healing activity comparable to that of the reference drug (Levomekol ointment). Conclusions. The selected substance-leader 1 in the composition of a model 5 % hydrophilic ointment based on sodium alginate exhibits pronounced biological activity and is a candidate for further research as a potential pharmaceutical substance with complex wound-healing and anti-inflammatory property.

scholarly journals Particularities of Experimental Models Used to Induce Gastric Ulcer

2019 ◽  
Vol 25 (4) ◽  
pp. 179-184
Author(s):  
Simona Fulga ◽  
Ana-Maria Pelin ◽  
Cristina Mihaela Ghiciuc ◽  
Elena Cătălina Lupușoru
Keyword(s):  
Gastric Ulcer ◽  
Hydrochloric Acid ◽  
Experimental Studies ◽  
Experimental Models ◽  
New Drugs ◽  
Laboratory Animals ◽  
Gastric Ulcers ◽  
Current Therapy ◽  
Surgical Methods

Abstract Introduction: Gastric ulcer is one of the most common gastrointestinal diseases, therefore the constant interest for new treatments is due to adverse effects induced by current therapy. The restricted number of in vivo experimental models is a challenge for researchers. Objectives: Identifying the particularities of different types of experimentally induced gastric ulcer in laboratory animals to facilitate their choise for the study of new antiulcer drugs. Material and method: A search in PubMed and Scopus using keywords ( “experimentally” AND “gastric ulcer” AND “rats/mice”) to include experimental studies with the description of local-induced changes. Review articles and in vitro studies were excluded. Results and discussions: Experimental researches on new drugs for gastric ulcer use chemical or surgical methods to induce gastric lesions in rats. Non-steroidal anti-inflammatory drugs (NSAIDs) and acetic acid models to investigate antisecretory and cytoprotective effects; ethanol models evaluate cytoprotective and/or antioxidant effects; pylorus ligature models to evaluate the effects on the secretion of aggressive gastric factors (hydrochloric acid or pepsin). NSAIDs (indomethacin, acetylsalicylic acid or ibuprofen) inhibit cyclooxygenase activity, resulting from reduced mucus and bicarbonate secretion, decreased mucosal blood flow, alteration of microvascular structures, causing epithelial damage Ethanol enhances the proteolytic and hydrolytic action of hydrochloric acid and pepsin; in addition, stimulates the acid secretion and disruptes vascular endothelium. Pylorus ligature determines the accumulation of gastric acid resulting in gastric ulcers due to the autodigestion of the mucosa. Conclusion: The knowledge of the mechanisms to induce experimental gastric ulcers is essential for choosing the model to evaluate new antiulcer agents.

scholarly journals Synthesis, Characterization and Anti-Diabetic Activity of 1,3,5-Triaryl-2-Pyrazolines in Acetic Acid Solution under Ultrasound Irradiation

2013 ◽  
Vol 14 ◽  
pp. 172-185 ◽  
Author(s):  
M. Emayavaramban ◽  
N. Santhi ◽  
C. Gopi ◽  
C. Manivannan ◽  
A. Raguraman
Keyword(s):  
Sodium Hydroxide Solution ◽  
Acetic Acid Solution ◽  
Ultrasound Irradiation ◽  
Temperature Treatment ◽  
Reference Drug ◽  
H Nmr ◽  
Phenylhydrazine Hydrochloride ◽  
Semicarbazide Hydrochloride ◽  
New Compounds

A chalcone was prepared by the reaction of 4-methylbenzaldehyde with 4-methylacetophenone in dilute methanolic sodium hydroxide solution under ultrasonic irradiationin the water bath of an ultrasonic cleaner at room temperature. Treatment of this chalcone with thiosemicarbazide/semicarbazide hydrochloride/benzhydrazide/benzenesulphonyl hydrazide/phenylhydrazine hydrochloride afforded the corresponding 2-pyrazoline in good yields. All the new compounds have been characterized by IR, 1H-NMR, 13CNMR spectral data. All the target compounds were evaluated for their In Vivo anti-diabetic activity in rates in comparison with as reference drug.

CORROSION ACTIVITY OF PENOX-1 DISINFECTANT

2021 ◽  
Vol 1 (1) ◽  
pp. 74-78
Author(s):  
A.M. Batyrova ◽  
Keyword(s):  
Stainless Steel ◽  
Sodium Hydroxide Solution ◽  
Steel Plates ◽  
Similar Data ◽  
Corrosion Activity ◽  
Corrosion Properties ◽  
Reference Drug ◽  
Metal Structures ◽  
Comparative Aspect ◽  
Metal Plates

One of the most important problems of the national economy is the protection of metal from corrosion, causing great damage to products and structures, shortening their useful life. Taking into account the importance of protecting metal structures of livestock objects from corrosion during disinfection work, the corrosion properties of the new Penox-1 disinfectant have been studied. Studies have shown that the tested drug «Penox-1» has a low corrosion activity in relation to metal products made of aluminum, galvanized iron and stainless steel, compared with the reference drug. Thus, the solution of the Penox-1 preparation reduced the initial weight of metal plates during 24 hours of exposure from aluminum by 0.196 g, which is 7.4%, and the standard preparation by 0.836 g or 32.1%, which is 4.3 times more . Similar data were obtained in a comparative aspect with galvanized iron and stainless steel plates. When examining metal plates after testing in a Penox-1 solution, the color and structure did not change visually and under a microscope. At that time, the plates immersed in a 2% sodium hydroxide solution changed strongly in color and structure, and a yellow-gray corrosive coating appeared.

scholarly journals P11.44 Conception of a promising future therapy: Drug loaded-microbubbles against glioblastoma

2019 ◽  
Vol 21 (Supplement_3) ◽  
pp. iii53-iii53
Author(s):  
E Schulz ◽  
V Mawamba ◽  
V Sturm ◽  
R Ernestus ◽  
U Schatzschneider ◽  
...  
Keyword(s):  
Real Time ◽  
Molecular Size ◽  
Chemotherapeutic Agents ◽  
New Drugs ◽  
Toxic Effects ◽  
Side Chains ◽  
Local Concentration ◽  
Tumor Site ◽  
Proliferation Assay ◽  
Reference Drug

Abstract BACKGROUND Major obstacles for an effective chemotherapy of glioblastomas (GBM) are the blood-brain-barrier (BBB) and serious systemic side effects of the cytotoxic drugs. A new promising strategy could be the delivery of microbubbles, encapsulating the chemotherapeutics, across the BBB to the tumor site. This will shield the drug from detrimental systemic effects. Low intensity focused ultrasound (LIFU) is able to open the BBB and triggers targeted release of the drugs within the tumor. First data on the synthesis of microbubbles, specifically designed new drugs and the targeted rupture of microbubbles by LIFU are presented. MATERIAL AND METHODS Thin-film hydration of lipids was utilized to prepare microbubbles, which were tested for toxicity on the GBM cell lines GaMG, U87, U138 and U343. In addition these cells were treated with 6 platinum(II) and palladium(II) complexes conjugated to lipophilic side chains of different length (C1, C8, C10) for 72h. To evaluate cell viability and calculate EC50 values MTT assays and a real-time proliferation assay using the impedance-based xCELLigence DP-System were executed. RESULTS Microbubbles ≤ 2µm in diameter were synthesized and could be disintegrated by applying LIFU. Neither the intact bubbles nor the lipids alone had any toxic effects on the GBM cells. In contrast, all six drugs were highly effective with EC50 values far below those of Temozolomide (67µM) and in the range of the reference drug cisplatin (3µM). Especially the palladium(II) compound with the C1-chain displayed a very low EC50 value (<10µM), while the longer chains and the platinum(II) compounds were less effective (EC50 10–40µM). An early and concentration-dependent onset of the cytotoxic effect of drugs with C1 and C8 side chains was revealed in the real time proliferation assay. CONCLUSION All components for a new microbubble-based therapeutic strategy are in place. Microbubbles were synthesized without having toxic effects in cell culture. New highly potent palladium(II) and platinum(II) compounds with low EC50 values were developed. The next step will be their encapsulation into the microbubbles via their lipophilic side chains to develop an effective drug-delivery system for the treatment of GBM in combination with LIFU. This will allow increasing the local concentration of chemotherapeutic agents at the tumor site, irrespectively of their molecular size and BBB penetration capacity.

scholarly journals SYSTEMATIC REVIEW: COCRYSTAL AS EFFORTS TO IMPROVE PHYSICOCHEMICAL AND BIOAVAILABILITY PROPERTIES OF ORAL SOLID DOSAGE FORM

2021 ◽  
pp. 43-52
Author(s):  
IYAN SOPYAN ◽  
ALVIN B. ◽  
INSAN SUNAN K. S. ◽  
CIKRA IKHDA N. H. S.
Keyword(s):  
Physicochemical Properties ◽  
Dosage Form ◽  
Water Solubility ◽  
Drug Stability ◽  
Water Soluble ◽  
New Drugs ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Water Soluble Drug ◽  
Biopharmaceutical Properties

Water solubility and low bioavailability of active pharmaceutical ingredients are some of the main challenges in the process of developing new drugs, especially drugs in oral solid dosage forms. One way to improve drug solubility is the principle of cocrystallization. Cocristallyzation itself is the process of combining the active ingredients of a less water-soluble drug with a coformer so that it becomes more soluble. Pharmaceutical cocrystal provides benefits to improve physicochemical properties without affecting its pharmacological properties. In this review, we have reviewed literature discussions and research that discuss co-crystallization as an aid to improve the physicochemical and bioavailability of drugs and also discuss some drugs in the form of cocrystal and their improvement in physicochemical-biopharmaceutical properties. The main references data used in this review are research journals published in the past 10 y (2010-2020) using keywords: cocrystal, physicochemistry, bioavailability, and solid dosage form, and using google scholar as a database. Discussion on the effect of cocrystal on physicochemical properties and bioavailability of drugs was produced. The method of producing cocrystal and its characterization was also discussed. Cocrystal offers a promising approach to improve the physicochemical properties of API. The benefits of cocrystal can be observed through increased solubility, dissolution rate, permeability, bioavailability, drug stability, and tabletability.

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